JPH03127739A - Alcohol absorption suppressant - Google Patents

Abstract

PURPOSE:To obtain the title suppressant controlling alcohol absorption from the stomach to blood, protecting organism from an evil influence of drinking, containing glycyl glycine as an active ingredient. CONSTITUTION:An alcohol absorption suppressant containing glycyl glycine as an active ingredient. In order to sufficiently exhibit inhibitory effects on alcohol absorption, a dose per time is preferably 0.5-5.0g, the suppressant is administered before drinking or simultaneously with drinking so that sickness caused by drinking and hangover are prevented and the suppressant is applied after drinking to prevent sickness caused by drinking and hangover.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Field of Application) The present invention relates to an alcohol absorption inhibitor containing glycyl glycine, which is a dipeptide, as an active ingredient. The preparation according to the present invention prevents an increase in blood alcohol concentration by suppressing the absorption of alcohol in the stomach, thereby protecting living bodies from the harmful effects of drinking alcohol.

(Prior Art) 20% of alcohol that enters the gastrointestinal tract is rapidly absorbed from the gastric mucosa and the rest from the small intestine, of which 5 to 10% is lost through exhalation and urine, but more than 90% is metabolized in the liver. In the liver, alcohol is oxidized to acetaldehyde by two enzyme systems, the alcohol dehydrogenase system and the microsomal ethanol oxidation system, which is then converted to acetic acid by acetaldehyde dehydrogenase. There are two types of acetaldehyde dehydrogenases with different Km values (dissociation constants of substrate-enzyme conjugates) (Reference 1), and acetaldehyde dehydrogenases with low Km values are involved in the oxidation of acetaldehyde. Approximately 50% of human livers contain atypical acetaldehyde dehydrogenase that lacks isozymes with low Km values for acetaldehyde (Reference 2).
．． 3) The acetaldehyde concentration in the blood of people with atypical acetaldehyde dehydrogenase after drinking alcohol is about 17 times higher than that of normal people (Reference 4). That is,
Since the enzyme does not act until the concentration of acetaldehyde in the blood is high, the oxidation of acetaldehyde is delayed, and its strong chemical reactivity and pharmacological toxic effects cause mainly circulatory problems such as facial flushing, increased heart rate, and increased skin temperature. In addition to pain due to abnormalities, symptoms such as headache, dizziness, drowsiness, nausea, and allergic symptoms may occur (Reference 5).

In recent years, the following reports have also been made regarding the side effects of alcohol and its oxide, acetaldehyde, associated with drinking.

(1) Due to inhibition of nerve cell membranes by alcohol (Na
" + to +) - Increased membrane fluidity due to suppression of ATPase activity and disorder of phospholipid sialic chains in the hydrophobic core of the membrane (Reference 6).

(2) Enzyme deviation due to necrosis of pancreatic cells due to direct metabolic disturbance of exocrine pancreatic gland cells caused by alcohol and the resulting breakdown of pancreatic duct branches (Reference 7).

(3) Hypertension due to promotion of catecholamine secretion by acetaldehyde, endocardial thrombus formation due to enhanced platelet aggregation, endocardial myocardial sclerosis, etc. (Reference 8).

(4) Various metabolic abnormalities, rotation of the citric acid cycle, and inhibition of fatty acid oxidation due to a decrease in the ability of liver mitochondria to oxidize acetaldehyde (Reference 9).

In order to drink alcoholic beverages in a healthy manner, it is desirable to reduce or neutralize the above-mentioned adverse effects on living organisms due to the toxicity of alcohol and its metabolite, acetaldehyde. From this point of view, various substances that reduce the concentration of alcohol or acetaldehyde in the blood or suppress the toxicity of acetaldehyde have been reported as described below.

Acetaldehyde trapping agent (1) D-penicillamine (Reference 10).

(2) S such as L-cysteine and DL-homocystine
H compound, vitamin B, its derivatives, and ascorbic acid (Reference 1).

(3) L-methionine (Reference 14).

Metabolism promoter (4) Egg white hydrolyzate (mixture of various amino acids) (Reference 1
2).

Toxicity reducer (5) L-α-alanine (Reference 13).

(Problems to be Solved by the Invention) The present inventor aims to prevent the increase in alcohol and acetaldehyde concentrations in the body by suppressing alcohol absorption from the gastrointestinal tract, thereby preventing acute toxicity, bad intoxication, and various other symptoms caused by alcohol intake. Thinking that it would be possible to suppress side effects, we searched for various substances that could suppress such alcohol absorption.

(Means for solving the problem) As a result, glycyl/glycine, a type of dipeptide, has the effect of suppressing the absorption of alcohol from the stomach into the blood. Therefore, if glycyl/glycine is administered, blood alcohol The present inventors have discovered that the increase in concentration can be prevented and the living body can be extremely effectively protected, leading to the completion of the present invention.

That is, the present invention provides an alcohol absorption inhibitor containing glycyl/glycine as an active ingredient.

Glycyl/glycine, which is the active ingredient of the present invention, is a simple dipeptide that does not contain an asymmetric carbon, and can be synthesized (Reference 15).
．． 16.17.18) or can be easily obtained from commercial products. In addition, it is tasteless and odorless, so even if it is mixed into various preparations, sensory aspects such as taste and smell will not be impaired, and it can be used with confidence. The formulation of the invention includes:
Organic acids such as citric acid and malic acid, inorganic salts such as sodium chloride and potassium chloride, vitamins, other amino acids, extracts of various herbal medicines, fragrances, etc. can be blended.

In addition to liquid formulations, the intake forms include powder formulations, granules,
Both tablets and capsules can be used.

Even if you drink the same amount of alcohol, the rate of absorption and metabolism varies greatly from person to person due to differences in body weight, constitution, etc., and although it is not possible to clearly define the effective amount of glycyl/glycine, it is effective in suppressing alcohol absorption. In order to achieve this effect, it is desirable that the single dose be in the range of 0.5 to 5.0 g.

There are no particular restrictions on when to take it; it can be taken before or at the same time as alcohol intake to prevent a hangover or a hangover, or it can be taken after alcohol intake to prevent a hangover.

The present invention will be explained in more detail with reference to test examples and production examples below.

Test Example 1 (1) Experimental animal: ddY conventional mouse, male, 4 to 5 weeks old.

(2) Experimental method Alcohol (ethyl alcohol) was diluted to 20% with distilled water. In addition, commercially available glycyl/glycine was dissolved in distilled water and tested as a 5-20% solution.

The mice were divided into a group to which alcohol was administered alone (control group) and a group to which alcohol and glycyl/glycine (5%, 10%, and 20%) were administered, and the mice were forcibly administered orally using a gastric tube.

First, glycyl glycine (4 to 4% as a 5-20% aqueous solution)
g/Kg) and 1 hour later alcohol (2 mQ/Kg as a 20% aqueous solution) was administered.

Distilled water (20 mQ/Km) was administered to mice in the control group instead of the test drug (glycyl/glycine).

One hour after the administration of alcohol, the animals were anesthetized with ether and underwent laparotomy, and blood samples were collected from the abdominal vena cava.

The stomach, including its contents, was also removed at the same time. After measuring the weight of the stomach, it was homogenized in purified water for 1 minute, and then the volume was adjusted to 40 mQ with purified water. 120 μQ of perchloric acid was added to 20 μa of each of the collected blood or homogenized solution, stirred, and centrifuged at 3000 rpm for 5 minutes, and the supernatants were used as blood and stomach samples. The alcohol concentration in the blood or stomach was measured by an enzymatic method (Reference 19).

In addition, Student's test was used as the criterion for determining effectiveness.

(3) Test results The blood and gastric alcohol concentrations determined by the enzyme method are shown in Figure 1. That is, the blood alcohol concentration of the glycyl/glycine administration group decreased as the dose increased, and the glycyl/glycine 20% solution showed significant inhibition with an inhibition rate of 84% (p<0°001). On the other hand, gastric alcohol concentration showed an inverse correlation. It was shown that the administration of Honjoku inhibited the absorption of alcohol, and the blood alcohol concentration was kept at a low level. This effect was dose dependent.

Production Example 1 [Liquid] Composition Glycyl/Glycine 5000111g Vitamin C6
00+++g Citric acid 200mg Fragrance 0,4 mQ Blend the above ingredients and add water to make the total amount 100m+2. It may also be used as a carbonated drink by blowing carbon dioxide gas into it.

Production Example 2 [Granule/Powder] Glycyl/Glycine 1000+++g Lactose
90mg Oxypropylcellulose 10mg Total 1100+++g After mixing in the above ratio, add a small amount of water and knead with a kneader, size the particles,
After drying, divide into packages. The above amount is considered to be one dose unit.

Production Example 3 [Tablets/Capsules] Glycyl/Glycine 300 mg Lactose 96+ni+Magnesium Stearate 4 mg Total 400 mg Glycyl/glycine and lactose are mixed in the above ratio and compressed into tablets. In the case of capsules, this is crushed, mixed with red sea bream stearate, and filled with a capsule filling machine. Take 2 or more doses at a time.

Kiln jar ■ Matsuda Yoshibe et al.: Alcohol metabolism and effects on the living body:
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Alcohol Metabolism and Liver Research Group Report, 223-234, 19
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[Brief explanation of the drawing]

FIG. 1 is a graph showing the influence of glycyl and glycine on blood and gastric alcohol concentrations. 3 Procedural amendment dated February 19, 1990

Claims (2)

[Claims] (1) Alcohol absorption inhibitor containing glycyl and glycine as active ingredients. (2) The formulation according to claim (1), which is orally administrable.